SB-216641

SB-216641
Clinical data
ATC code	none;
Identifiers
	IUPAC name N-[3-[3-(dimethylamino)ethoxy]-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide;
CAS Number	170230-39-4 ;
PubChem CID	3292447;
IUPHAR/BPS	28;
ChemSpider	2541153;
CompTox Dashboard (EPA)	DTXSID4043985 ;
Chemical and physical data
Formula	C28H30N4O4
Molar mass	486.561 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN(C)CCOc1cc(ccc1OC)NC(=O)c3ccc(cc3)-c2ccc(cc2C)-c4noc(C)n4;
	InChI InChI=1S/C28H30N4O4/c1-18-16-22(27-29-19(2)36-31-27)10-12-24(18)20-6-8-21(9-7-20)28(33)30-23-11-13-25(34-5)26(17-23)35-15-14-32(3)4/h6-13,16-17H,14-15H2,1-5H3,(H,30,33); Key:JRNUKVFYILMMLX-UHFFFAOYSA-N;
(verify)

SB-216641 is a drug which is a selective antagonist for the serotonin receptor 5-HT_1B, with around 25x selectivity over the closely related 5-HT_1D receptor.[1] It is used in scientific research,[2][3][4] and has demonstrated anxiolytic effects in animal studies.[5][6]

References

Price, GW; Burton, MJ; Collin, LJ; Duckworth, M; Gaster, L; Göthert, M; Jones, BJ; Roberts, C; et al. (1997). "SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 356 (3): 312–20. doi:10.1007/PL00005056. PMID 9303567.
Matsuoka, T; Hasuo, H; Akasu, T (2004). "5-Hydroxytryptamine 1B receptors mediate presynaptic inhibition of monosynaptic IPSC in the rat dorsolateral septal nucleus". Neuroscience research. 48 (3): 229–38. doi:10.1016/j.neures.2003.11.004. PMID 15154669.
Yan, QS; Zheng, SZ; Yan, SE (2004). "Involvement of 5-HT1B receptors within the ventral tegmental area in regulation of mesolimbic dopaminergic neuronal activity via GABA mechanisms: a study with dual-probe microdialysis". Brain Research. 1021 (1): 82–91. doi:10.1016/j.brainres.2004.06.053. PMID 15328035.
Lee, JJ; Hahm, ET; Lee, CH; Cho, YW (2008). "Serotonergic modulation of GABAergic and glutamatergic synaptic transmission in mechanically isolated rat medial preoptic area neurons". Neuropsychopharmacology. 33 (2): 340–52. doi:10.1038/sj.npp.1301396. PMID 17392733.
Tatarczyńska, E; Kłodzińska, A; Stachowicz, K; Chojnacka-Wójcik, E (2004). "Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression". Behavioural Pharmacology. 15 (8): 523–34. doi:10.1097/00008877-200412000-00001. PMID 15577451.
Chojnacka-Wójcik, E; Kłodzińska, A; Tatarczyńska, E (2005). "The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action". The Journal of Pharmacy and Pharmacology. 57 (2): 253–7. doi:10.1211/0022357055399. PMID 15720791.

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[1] Price, GW; Burton, MJ; Collin, LJ; Duckworth, M; Gaster, L; Göthert, M; Jones, BJ; Roberts, C; et al. (1997). "SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 356 (3): 312–20. doi:10.1007/PL00005056. PMID 9303567.

[2] Matsuoka, T; Hasuo, H; Akasu, T (2004). "5-Hydroxytryptamine 1B receptors mediate presynaptic inhibition of monosynaptic IPSC in the rat dorsolateral septal nucleus". Neuroscience research. 48 (3): 229–38. doi:10.1016/j.neures.2003.11.004. PMID 15154669.

[3] Yan, QS; Zheng, SZ; Yan, SE (2004). "Involvement of 5-HT1B receptors within the ventral tegmental area in regulation of mesolimbic dopaminergic neuronal activity via GABA mechanisms: a study with dual-probe microdialysis". Brain Research. 1021 (1): 82–91. doi:10.1016/j.brainres.2004.06.053. PMID 15328035.

[4] Lee, JJ; Hahm, ET; Lee, CH; Cho, YW (2008). "Serotonergic modulation of GABAergic and glutamatergic synaptic transmission in mechanically isolated rat medial preoptic area neurons". Neuropsychopharmacology. 33 (2): 340–52. doi:10.1038/sj.npp.1301396. PMID 17392733.

[5] Tatarczyńska, E; Kłodzińska, A; Stachowicz, K; Chojnacka-Wójcik, E (2004). "Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression". Behavioural Pharmacology. 15 (8): 523–34. doi:10.1097/00008877-200412000-00001. PMID 15577451.

[6] Chojnacka-Wójcik, E; Kłodzińska, A; Tatarczyńska, E (2005). "The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action". The Journal of Pharmacy and Pharmacology. 57 (2): 253–7. doi:10.1211/0022357055399. PMID 15720791.